Tips for: Solid Oral Dosage Forms

Many active pharmaceutical ingredients (APIs) exhibit poor solubility in conventional solvents, which can significantly affect the formulation and bioavailability of the drug. This is particularly challenging when developing soft gelatin capsules, as achieving sufficient solubility is essential for the drug to be effectively absorbed in the gastrointestinal tract. The limited availability of suitable solvents for poorly soluble drugs often requires the use of advanced techniques and the careful selection of excipients to achieve adequate solubilization without compromising the drug’s stability, safety, or efficacy.
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Developing a soft gelatin capsule formulation at the pilot scale can be an expensive process, especially for new drug candidates or novel formulations. The costs associated with pilot-scale development include raw materials, equipment, testing, and labor, all of which contribute to the high expenses. Additionally, when dealing with specialized formulations, such as those with low doses, complex release profiles, or sensitive APIs, the process can become even more costly. These expenses can create significant barriers for smaller pharmaceutical companies or organizations working with limited budgets, impacting their ability to bring innovative products to market efficiently.
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Diluents, also known as fillers, are critical excipients in hard gelatin capsule formulations. They are used to increase the volume of the capsule and ensure that the correct dose of the active pharmaceutical ingredient (API) is delivered. However, selecting the optimal diluent is often challenging because it must not only be compatible with the API but also with other excipients used in the formulation. The choice of diluent can affect the mechanical strength, dissolution rate, and stability of the final product. Choosing the wrong diluent can lead to issues such as poor flow properties, inconsistent fill weights, or reduced bioavailability of the drug.
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Formulating suspensions for encapsulation in soft gelatin capsules presents unique challenges, particularly when dealing with poorly soluble active pharmaceutical ingredients (APIs). Suspensions are formulations in which the API is dispersed in a liquid, and these systems are commonly used when the drug does not dissolve well in water or other solvents. However, when attempting to encapsulate these suspensions in soft gelatin capsules, several issues arise, including maintaining uniformity of the suspension, preventing phase separation, and ensuring consistent fill volumes. These challenges require careful formulation strategies to ensure that the suspension remains stable, and that the API is delivered effectively and consistently over time.
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Encapsulating volatile compounds in soft gelatin capsules presents unique challenges due to their tendency to evaporate, degrade, or alter the properties of the capsule shell. Volatile compounds are often essential for the therapeutic action of certain drugs, such as in the case of essential oils, some pharmaceutical agents, and fragrance compounds. However, the encapsulation process must be carefully controlled to avoid the loss of the active ingredient and ensure the stability, safety, and efficacy of the final product. The volatile nature of these compounds may also impact the capsule’s integrity, leading to issues like leakage, shell softening, or compromised release profiles.
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Soft gelatin capsules are commonly used for drug delivery, but they face challenges when the API content is low. In cases where the active pharmaceutical ingredient (API) content is minimal, there are constraints on the shell thickness required to ensure the integrity, stability, and release of the capsule. If the shell is too thick, the capsule may be too large or uncomfortable for patients to swallow. On the other hand, if the shell is too thin, it may not provide adequate protection to the drug or may lead to leakage or other issues during manufacturing, storage, and use. Balancing shell thickness while maintaining proper API stability and drug release can be difficult, especially in formulations with low drug content.
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Achieving the desired drug release profile in hard gelatin capsules is a significant challenge in pharmaceutical formulation development. The release profile of a drug is crucial to its therapeutic effectiveness, and it must be tailored to meet specific patient needs. Targeted release profiles are often required for drugs that need to be delivered at particular sites in the gastrointestinal tract or at a specific time after administration. However, formulating hard gelatin capsules with precise and predictable release profiles can be difficult due to various factors such as API solubility, excipient interactions, and the capsule shell’s dissolution characteristics.
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